TWI729169B - 乙炔基衍生物 - Google Patents

乙炔基衍生物 Download PDF

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Publication number
TWI729169B
TWI729169B TW106123741A TW106123741A TWI729169B TW I729169 B TWI729169 B TW I729169B TW 106123741 A TW106123741 A TW 106123741A TW 106123741 A TW106123741 A TW 106123741A TW I729169 B TWI729169 B TW I729169B
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Taiwan
Prior art keywords
formula
compound
methyl
compounds
dihydro
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TW106123741A
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English (en)
Chinese (zh)
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TW201805287A (zh
Inventor
芭芭拉 比曼斯
喬治 傑許柯
安東尼歐 瑞奇
丹尼爾 路荷
費歐恩 歐哈拉
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瑞士商赫孚孟拉羅股份公司
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/527—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim spiro-condensed
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/09—Geometrical isomers
TW106123741A 2016-07-18 2017-07-17 乙炔基衍生物 TWI729169B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
??16179837.6 2016-07-18
EP16179837.6 2016-07-18
EP16179837 2016-07-18

Publications (2)

Publication Number Publication Date
TW201805287A TW201805287A (zh) 2018-02-16
TWI729169B true TWI729169B (zh) 2021-06-01

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TW106123741A TWI729169B (zh) 2016-07-18 2017-07-17 乙炔基衍生物

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US (3) US20190144458A1 (ru)
EP (1) EP3484889B1 (ru)
JP (1) JP6936305B2 (ru)
KR (1) KR20190026805A (ru)
CN (1) CN109476671B (ru)
AR (1) AR109075A1 (ru)
AU (1) AU2017299083B2 (ru)
BR (1) BR112019000314A2 (ru)
CA (1) CA3030788A1 (ru)
CL (1) CL2019000045A1 (ru)
CO (1) CO2018013824A2 (ru)
CR (1) CR20190014A (ru)
DK (1) DK3484889T3 (ru)
ES (1) ES2826389T3 (ru)
HR (1) HRP20201615T1 (ru)
HU (1) HUE051006T2 (ru)
IL (1) IL263884A (ru)
LT (1) LT3484889T (ru)
MA (1) MA45665B1 (ru)
MX (1) MX2019000442A (ru)
PE (1) PE20190382A1 (ru)
PH (1) PH12019500119A1 (ru)
PL (1) PL3484889T3 (ru)
PT (1) PT3484889T (ru)
RS (1) RS60908B1 (ru)
RU (1) RU2745068C2 (ru)
SG (1) SG11201811829QA (ru)
SI (1) SI3484889T1 (ru)
TW (1) TWI729169B (ru)
WO (1) WO2018015235A1 (ru)
ZA (1) ZA201900113B (ru)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107580598B (zh) 2015-07-15 2020-11-13 豪夫迈·罗氏有限公司 作为代谢型谷氨酸受体调节剂的乙炔基衍生物
CN110183456A (zh) * 2019-07-11 2019-08-30 河南师范大学 一种2-芳基吲唑琥珀酰亚胺螺环化合物的合成方法
US11515154B2 (en) * 2020-10-27 2022-11-29 Applied Materials, Inc. Selective deposition of a passivation film

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WO2015128307A1 (en) * 2014-02-25 2015-09-03 F. Hoffmann-La Roche Ag Ethynyl derivatives
WO2017009275A1 (en) * 2015-07-15 2017-01-19 F. Hoffmann-La Roche Ag Ethynyl derivatives as metabotropic glutamate receptor modulators

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AU2003298889A1 (en) * 2002-12-04 2004-06-23 Merck & Co., Inc. Spirocyclic ureas, compositions containing such compounds and methods of use
UA90145C2 (ru) 2005-05-24 2010-04-12 Лаборатуар Сероно С.А. Трициклические спиро-производные как модуляторы crth2
CN101528711A (zh) 2006-08-31 2009-09-09 先灵公司 可用作抗细菌剂的乙内酰脲衍生物
WO2008151184A1 (en) 2007-06-03 2008-12-11 Vanderbilt University Benzamide mglur5 positive allosteric modulators and methods of making and using same
WO2011029104A1 (en) 2009-09-04 2011-03-10 Vanderbilt University Mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
US8389536B2 (en) 2009-10-27 2013-03-05 Hoffmann-La Roche Inc. Positive allosteric modulators (PAM)
US8759377B2 (en) 2009-11-23 2014-06-24 Vanderbilt University Substituted dioxopiperidines and dioxopyrrolidines as MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
US8586581B2 (en) * 2009-12-17 2013-11-19 Hoffmann-La Roche Inc Ethynyl compounds useful for treatment of CNS disorders
US8420661B2 (en) 2010-04-13 2013-04-16 Hoffmann-La Roche Inc. Arylethynyl derivatives
US8772300B2 (en) 2011-04-19 2014-07-08 Hoffmann-La Roche Inc. Phenyl or pyridinyl-ethynyl derivatives
HUE025031T2 (en) 2011-04-26 2016-02-29 Hoffmann La Roche Ethinyl derivatives as positive allosteric modulators of MGLUR5
US10533000B2 (en) 2011-05-26 2020-01-14 Sunovion Pharmaceuticals, Inc. Metabotrophic glutamate receptor 5 modulators and methods of use thereof
JP6205354B2 (ja) * 2011-07-06 2017-09-27 ギリアード サイエンシーズ， インコーポレイテッド Ｈｉｖの処置のための化合物
US20130123254A1 (en) 2011-09-30 2013-05-16 Barbara Biemans Pharmaceutically acceptable mglur5 positive allosteric modulators and their methods of identification
UA110862C2 (uk) 2011-10-07 2016-02-25 Ф. Хоффманн-Ля Рош Аг Похідні етинілу як алостеричні модулятори метаботропного рецептора глутамату mglur 5
NZ703537A (en) 2012-10-18 2018-06-29 Hoffmann La Roche Ethynyl derivatives
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CN105121424B (zh) 2013-02-18 2019-01-22 华领医药技术（上海）有限公司 mGluR调节剂
UY35400A (es) 2013-03-15 2014-10-31 Novartis Ag Compuestos y composiciones para el tratamiento de enfermedades parasitarias
JO3368B1 (ar) 2013-06-04 2019-03-13 Janssen Pharmaceutica Nv مركبات 6، 7- ثاني هيدرو بيرازولو [5،1-a] بيرازين- 4 (5 يد)- اون واستخدامها بصفة منظمات تفارغية سلبية لمستقبلات ميجلور 2
TWI649310B (zh) 2014-01-10 2019-02-01 赫孚孟拉羅股份公司 乙炔基衍生物
CN104860941B (zh) 2014-02-25 2017-03-22 上海海雁医药科技有限公司 2,4‑二取代苯‑1,5‑二胺衍生物及其应用以及由其制备的药物组合物和药用组合物
WO2016146600A1 (en) 2015-03-19 2016-09-22 F. Hoffmann-La Roche Ag 3-(4-ethynylphenyl)hexahydropyrimidin-2,4-dione derivatives as modulators of mglur4
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Patent Citations (3)

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WO2015044075A1 (en) * 2013-09-25 2015-04-02 F. Hoffmann-La Roche Ag Ethynyl derivatives
WO2015128307A1 (en) * 2014-02-25 2015-09-03 F. Hoffmann-La Roche Ag Ethynyl derivatives
WO2017009275A1 (en) * 2015-07-15 2017-01-19 F. Hoffmann-La Roche Ag Ethynyl derivatives as metabotropic glutamate receptor modulators

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Publication number Publication date
US20190144458A1 (en) 2019-05-16
PE20190382A1 (es) 2019-03-08
PT3484889T (pt) 2020-10-15
CL2019000045A1 (es) 2019-06-07
AR109075A1 (es) 2018-10-24
MX2019000442A (es) 2019-06-20
DK3484889T3 (da) 2020-10-26
SG11201811829QA (en) 2019-02-27
PH12019500119A1 (en) 2019-12-11
IL263884A (en) 2019-01-31
AU2017299083B2 (en) 2021-06-24
RS60908B1 (sr) 2020-11-30
CN109476671A (zh) 2019-03-15
US20220127275A1 (en) 2022-04-28
EP3484889B1 (en) 2020-08-19
US20200255440A1 (en) 2020-08-13
US11242349B2 (en) 2022-02-08
CO2018013824A2 (es) 2018-12-28
JP2019521158A (ja) 2019-07-25
PL3484889T3 (pl) 2020-12-28
CR20190014A (es) 2019-03-04
MA45665B1 (fr) 2020-11-30
TW201805287A (zh) 2018-02-16
WO2018015235A1 (en) 2018-01-25
CN109476671B (zh) 2021-09-24
CA3030788A1 (en) 2018-01-25
RU2019102757A3 (ru) 2020-08-18
RU2745068C2 (ru) 2021-03-18
AU2017299083A1 (en) 2019-01-24
EP3484889A1 (en) 2019-05-22
HUE051006T2 (hu) 2021-01-28
ES2826389T3 (es) 2021-05-18
JP6936305B2 (ja) 2021-09-15
RU2019102757A (ru) 2020-08-18
KR20190026805A (ko) 2019-03-13
HRP20201615T1 (hr) 2020-12-11
BR112019000314A2 (pt) 2019-04-16
SI3484889T1 (sl) 2020-11-30
LT3484889T (lt) 2020-11-10
ZA201900113B (en) 2019-09-25

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